Gastrointestinal System

and Nutrition
Antacids Antidiarrheals
Histamine-2 (H2)-receptor antago- Agents for dissolution of gallstones
nists Agents for inflammatory bowel dis-
Muscarinic receptor antagonists ease
Proton-pump inhibitors Agents for portal system encephal-
Mucosal protective agents opathy
Pancreatic replacement enzymes Vitamins
Laxatives

Questions
DIRECTIONS: Each item below contains a question or incomplete
statement followed by suggested responses. Select the one best response to
each question.

382. Cimetidine slows the metabolism of many drugs because it inhibits

the activity of
a. Monoamine oxidase (MAO)
b. Cytochrome P450
c. Tyrosine kinase
d. Hydrogen–potassium–adenosine triphosphatase (H+,K+,ATPase)
e. Phase II glucuronidation reactions

383. The absorption of phosphate is reduced when large and prolonged

doses of which of the following antacids are given?
a. Na bicarbonate
b. Mg hydroxide
c. Mg trisilicate
d. Ca carbonate
e. Sucralfate

215

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216 Pharmacology

384. Omeprazole, an agent for the promotion of healing of peptic ulcers,

has a mechanism of action that is based on
a. Prostaglandins
b. Gastric secretion
c. Pepsin secretion
d. H+,K+,ATPase
e. Anticholinergic action

385. An effective antidiarrheal agent that inhibits peristaltic movement is

a. Clonidine
b. Bismuth subsalicylate
c. Oral electrolyte solution
d. Atropine
e. Diphenoxylate

386. The approved indication for misoprostol

a. Reflux esophagitis
b. Regional ileitis
c. Ulcerative colitis
d. Prevention of gastric ulceration in patients using large doses of aspirin-like
drugs
e. Pathologic hypersecretory conditions such as Zollinger-Ellison syndrome

387. Metoclopramide has antiemetic properties because it

a. Accelerates gastric emptying time
b. Lowers esophageal sphincter pressure
c. Is a central nervous system (CNS) dopamine-receptor antagonist
d. Has cholinomimetic properties
e. Has sedative properties

388. The steatorrhea of pancreatic insufficiency can best be treated by

a. Cimetidine
b. Misoprostol
c. Bile salts
d. Pancrelipase
e. Secretin
 Gastrointestinal System and Nutrition 217

389. Cholesterol gallstones may be dissolved by oral treatment with

a. Lovastatin
b. Dehydrocholic acid
c. Methyl tertiary butyl ether
d. Chenodeoxycholic acid
e. Monoctanoin

390. A drug of choice in the therapy of inflammatory bowel disease is

a. Sulfadiazine
b. Sulfasalazine
c. Sulfapyridine
d. Sulfamethoxazole
e. Salicylate sodium

391. An important drug in the therapy of portal systemic encephalopathy is

a. Lactulose
b. Lactate
c. Loperamide
d. Lorazepam
e. Loxapine

392. Bismuth salts are thought to be effective in peptic ulcer disease because
they have bactericidal properties against
a. Escherichia coli
b. Bacteroides fragilis
c. Clostridium difficile
d. Helicobacter pylori
e. Staphylococcus aureus

393. Misoprostol has a cytoprotective action on the gastrointestinal (GI)

mucosa because it
a. Enhances secretion of mucus and bicarbonate ion
b. Neutralizes acid secretion
c. Antagonizes nonsteroidal anti-inflammatory drugs (NSAIDs)
d. Relieves ulcer symptoms
e. Coats the mucosa
218 Pharmacology

394. For the severe form of nodulocystic acne vulgaris, the first line of
therapy is the systemic use of
a. Vitamin A
b. Retinol
c. Tetracycline
d. Isotretinoin (13-cis-retinoic acid)
e. Ciprofloxacin

395. The primary pharmacologic action of omeprazole is the reduction of

a. Volume of gastric juice
b. Gastric motility
c. Secretion of pepsin
d. Secretion of gastric acid
e. Secretion of intrinsic factor

396. Which of the following vitamins in large doses is teratogenic?

a. Vitamin A
b. Vitamin B12
c. Vitamin C
d. Vitamin D
e. Vitamin E

397. Fat-soluble vitamins generally have a greater potential toxicity com-

pared with water-soluble vitamins because they are
a. More essential to vital metabolic processes
b. Metabolically faster
c. Avidly stored by the body
d. Administered in larger doses
e. Involved in more essential metabolic pathways

398. In the United States, the recommended daily allowances (RDAs) are
periodically developed by the
a. National Research Council (NRC)
b. Food and Drug Administration (FDA)
c. Department of Agriculture
d. Department of Commerce
e. Surgeon General
 Gastrointestinal System and Nutrition 219

399. Which vitamin needs to be given in supplemental doses in order to

prevent deficiency when a patient is given prolonged administration of iso-
niazid (INH)?
a. Vitamin A
b. Vitamin K
c. Vitamin C
d. Thiamine
e. Pyridoxine

400. Which of the following is a stool softener that has no effect on

absorption of fat-soluble vitamins?
a. Mineral oil
b. Castor oil
c. Docusate sodium
d. Phenolphthalein
e. Cascara sagrada

401. Which of the following is not associated with sucralfate?

a. It contains polyaluminum hydroxide
b. It maintains gellike qualities even at acid pH
c. It binds to ulcer craters more than to normal mucosae
d. It has moderate acid-neutralizing properties
e. It reacts very little with mucin
220 Pharmacology

DIRECTIONS: Each group of questions below consists of lettered

options followed by a set of numbered items. For each numbered item,
select the one lettered option with which it is most closely associated. Each
lettered option may be used once, more than once, or not at all.

Questions 402–403
Match each vitamin with the appropriate description.
a. Excess amounts should be avoided when the patient is on levodopa (L-dopa)
b. Overdosage may lead to a psychotic state
c. Improvement of vision especially in daylight might be attributable to this vitamin
d. This vitamin is usually not included in the popular one-a-day vitamin prepara-
tions
e. Retinoic acid is the natural form
f. Acute intoxication with this vitamin causes hypertension, nausea, and vomit-
ing, and signs of increased cerebrospinal fluid (CSF) pressure
g. This vitamin has hormonal functions
h. This fat-soluble vitamin has mainly antioxidant properties
i. In its water-soluble form, this fat-soluble vitamin is capable of producing ker-
nicterus

402. Calcitriol (vitamin D metabolite—1,25-dihydroxyvitamin D)

403. Pyridoxine

Questions 404–405
For each vitamin, match the appropriate use or deficiency.
a. Large doses are used to treat hyperlipoproteinemia
b. Large doses are used to acidify urine
c. This vitamin is used in the therapy of Wernicke’s syndrome
d. Large doses are used to cure psychosis
e. Deficiency can cause angular stomatitis
f. Deficiency can cause the common cold
g. Deficiency can cause convulsions in children

404. Riboflavin

405. Thiamine
 Gastrointestinal System and Nutrition 221

Questions 406–407
Match the main therapeutic potential with the correctly listed GI drug.
a. Ranitidine
b. Metronidazole
c. Omeprazole
d. Sucralfate
e. Misoprostol
f. Ca carbonate
g. Loperamide

406. Preferred drug therapy for Zollinger-Ellison syndrome

407. Helpful in selected cases of diarrhea

Questions 408–409
There are different mechanisms by which laxatives achieve their effects.
Match the mechanism to the correct drug.
a. Mg sulfate
b. Methylcellulose
c. Phenolphthalein
d. Castor oil
e. Lactulose
f. Mineral oil
g. Docusate Na (dioctyl sodium sulfosuccinate)

408. Has a hyperosmotic mechanism different from that of saline cathartics

409. Increases colonic peristalsis and enhances fluid and electrolyte secre-
tion into the bowel
222 Pharmacology

Questions 410–411
A large number of endogenous and exogenous agents act to alter the rate of
acid secretion by the parietal cell. Match the mechanism to the agent.
a. Histamine
b. Gastrin
c. Acetylcholine (ACh)
d. Aspirin
e. Food
f. Al hydroxide
g. Bismuth subsalicylate
h. Omeprazole
i. Misoprostol
j. Sucralfate

410. Lowers gastric secretion and is contraindicated in women of child-

bearing age

411. Increases gastric acidity by preventing the action of inhibitory gua-

nine nucleotide-binding protein (G protein) on adenylate cyclase
Gastrointestinal System
and Nutrition
Answers
382. The answer is b. (Hardman, p 906.) Cimetidine reversibly inhibits
cytochrome P450. This is important in phase I biotransformation reactions
and inhibits the metabolism of such drugs as warfarin, phenytoin, propra-
nolol, metoprolol, quinidine, and theophylline. None of the other enzymes
are significantly affected.

383. The answer is d. (Katzung, pp 1064–1066.) Although Al hydroxide

is generally considered to be the antacid that inhibits phosphate absorp-
tion, Ca carbonate is equally capable of this effect. This adverse effect may
be hazardous in the presence of renal impairment.

384. The answer is d. (Hardman, pp 907–909.) Omeprazole inhibits

H+,K+,ATPase, which effectively stops the proton pump and thus prevents
the formation of gastric acid. It is the most effective agent in severe cases of
ulceration and esophageal reflux.

385. The answer is e. (Hardman, p 926.) Diphenoxylate is a piperidine

opioid that is related to meperidine. It inhibits peristalsis and, hence,
increases the passage time of the intestinal bolus. It is combined with
atropine to discourage use as a street drug. Atropine has little effect on peri-
stalsis. Clonidine, bismuth subsalicylate, and rehydration therapy are all
useful in some types of diarrhea, but none of them inhibit peristalsis.

386. The answer is d. (Hardman, p 611.) Misoprostol is a prostaglandin E

(PGE) analogue that has antisecretory and mucosal protection properties in
the stomach. Experimentally, it protects against mucosal damage from
NSAIDs, alcohol, and other toxic agents. It will also tend to heal existing
ulcers, but it is inferior to other agents in this regard.

387. The answer is c. (Hardman, pp 932–933.) Metoclopramide antago-

nizes the emetic effect of apomorphine, which is mediated by a dopamine

223
224 Pharmacology

receptor in the CNS. It also raises the lower esophageal sphincter pressure
and relaxes the pyloric sphincter, which hastens gastric emptying time.
This makes it useful in the therapy of reflux esophagitis.

388. The answer is d. (Hardman, p 935.) Pancrelipase is an alcoholic

extract of hog pancreas that contains lipase, trypsin, and amylase. It is
effective in reducing the steatorrhea of pancreatic insufficiency. None of the
other drugs mentioned have significant action in the digestion of fats.

389. The answer is d. (Hardman, pp 934–935.) Chenodeoxycholic acid

(chenodiol) and ursodiol have proved to be effective in some patients with
cholesterol gallstones. Lovastatin lowers blood cholesterol levels but has
no effect on gallstones. Methyl tertiary butyl ether and a new agent,
monoctanoin, are infused directly into the common duct and will dissolve
gallstones.

390. The answer is b. (Hardman, p 1061.) Sulfasalazine consists of sul-

fapyridine with 5-aminosalicylic acid linked by an azo- bond. This bond
is broken by bacteria that release the salicylic acid, which is believed to be
the active agent. Sulfa drugs or salicylic acid used alone is not as effective.
The mechanism of action is unknown, but it is believed to be protective
action on the mucosa by inhibition of the synthesis of prostaglandins and
leukotrienes.

391. The answer is a. (Hardman, p 922.) Lactulose is a synthetic di-

saccharide (galactose-fructose) that is not absorbed. In moderate doses, it
acts as a laxative. In higher doses, it is capable of binding ammonia and
other toxins that form in the intestine in severe liver deficiency and that are
believed to cause the encephalopathy. Loperamide is an antidiarrheal opi-
oid; lorazepam is a CNS depressant; loxapine is a heterocyclic antipsychotic.

392. The answer is d. (Hardman, pp 909–910.) It is now recognized that

infection with H. pylori is a major etiologic factor in peptic ulcer disease.
Bismuth salts are bactericidal for many organisms but especially for spiro-
chetes. Colloidal bismuth salts such as bismuth subsalicylate also have a
coating or cytoprotective action. Antimicrobials and GI antisecretory drugs
are also used in combination with bismuth compounds.
 Gastrointestinal System and Nutrition Answers 225

393. The answer is a. (Hardman, p 914.) Misoprostol is a prostaglandin

analogue of PGE with an affinity for the gastric mucosa. It stimulates
the secretion of mucus and bicarbonate, enhances cell proliferation, pre-
serves the microcirculation, and stabilizes tissue lysosomes. Misoprostol is
approved by the FDA for protection against the ulcerogenic action of
NSAIDs (not because it antagonizes NSAIDs).

394. The answer is d. (Hardman, p 1575.) Isotretinoin is actually a form

of high-dose vitamin A therapy. Vitamin A itself or retinol (vitamin A1)
could be used, but they have less advantageous pharmacokinetic proper-
ties. Antibiotics such as tetracyclines are used in acne, but they have little
effect on the nodulocystic form.

395. The answer is d. (Hardman, pp 907–909.) The main action of

omeprazole is the inhibition of secretion of gastric acid. Because it is a spe-
cific inhibitor of the proton pump (H+,K+,ATPase), other actions are sec-
ondary to the marked decline of acid secretion. As a result of the reduction
of gastric acidity, there is increased secretion of gastrin leading to hyper-
gastrinemia.

396. The answer is a. (Hardman, p 1579.) Pregnant women should not

take more than a 25% increase in the normal dietary intake of vitamin A,
because it is definitely teratogenic, especially in the first trimester of preg-
nancy. Great caution is to be taken in premenopausal females in the ther-
apy of acne and skin wrinkling in which tretinoin or isotretinoin is the
therapeutic agent. None of the other vitamins is particularly teratogenic,
except perhaps vitamin D.

397. The answer is c. (Hardman, pp 1578–1579, 1533.) Fat-soluble vita-

mins, especially vitamins A and D, can be stored in massive amounts and,
hence, have a potential for serious toxicities. Water-soluble vitamins are
easily excreted by the kidney and toxic accumulation rarely occurs.

398. The answer is a. (Hardman, pp 1547–1542.) The NRC has a Food

and Nutrition Board, which has the function of selecting the levels of vita-
mins, minerals, and other substances that are necessary to achieve maximum
nutritional health. The levels are reviewed periodically and determined by
226 Pharmacology

study of the nutritional needs of healthy persons. The FDA is responsible for
the labeling of nutritional products, but it does not determine the RDAs.

399. The answer is e. (Hardman, p 1563.) The toxicity of INH is mainly

on the peripheral and central nervous systems (PNS, CNS). This is attrib-
utable to competition of INH with pyridoxal phosphate for apotryp-
tophanase. This results in a relative deficiency of pyridoxine, which causes
peripheral neuritis, insomnia, and muscle twitching among other effects.

400. The answer is c. (Hardman, p 924.) Dioctyl sodium sulfosuccinate

(docusate) is a detergent that, when given orally, softens the stool and pre-
vents straining. Mineral oil also softens the stool, but it tends to inhibit the
absorption of fat-soluble vitamins and other nutrients. Castor oil, phenol-
phthalein, and cascara sagrada are strong laxatives and cause watery stools.

401. The answer is d. (Hardman, p 913.) Sucralfate is a sulfated disac-

charide that contains polyaluminum hydroxide. It has primarily protective
properties and attaches firmly to ulcer craters. It has no significant acid-
neutralizing properties.

402–403. The answers are 402-g, 403-a. (Hardman, pp 1529–1532,

1582–1585.) Calcitriol (1,25-dihydroxyvitamin D) is the most active form
of vitamin D. It is formed by the kidney. When the Ca blood level rises, the
kidney produces 24,25-dihydroxyvitamin D, a much less active form. Vita-
min D can be manufactured in the body by the action of sunlight on the
skin. Its main action is to increase Ca absorption in the gut. Thus, vitamin
D subserves important hormonal functions in Ca homeostasis.
Levodopa is converted to dopamine in the peripheral tissues by dopa
decarboxylase, which has pyridoxine as a cofactor. Excess of this vitamin will
increase this reaction, which is an undesirable effect because dopamine does
not cross the blood-brain barrier where the therapeutic effect is desired.

404–405. The answers are 404-e, 405-c. (Hardman, pp 1555–1557,

1559–1561.) Angular stomatitis, dermatitis, and corneal vascularization are
considered classic signs of human riboflavin deficiency, although multiple B
vitamins may be involved.
The classic therapy of the bizarre CNS signs and symptoms of with-
drawal in severe alcoholics (Wernicke’s syndrome) is intravenous adminis-
 Gastrointestinal System and Nutrition Answers 227

tration of thiamine plus glucose infusion. Alcoholics generally have other

deficiencies of vitamins, especially riboflavin and niacin.

406–407. The answers are 406-c, 407-g. (Hardman, pp 907–909, 926–

927.) Omeprazole, which is an inhibitor of the parietal cell H+,K+,ATPase
pump (proton pump), is the most effective means of decreasing gastric acid-
ity. This makes it the ideal agent to treat Zollinger-Ellison syndrome, which
results from increased gastric secretion due to gastrinomas.
Loperamide is an opiate that is poorly absorbed from the GI tract but
still retains the ability to inhibit peristalsis. It is useful in diarrheas that are
just symptomatic and are not due to infection or organic pathology, such as
inflammatory bowel disease.

408–409. The answers are 408-e, 409-c. (Hardman, pp 922–923.) Lactu-

lose is a disaccharide that is not absorbed and, thus, acts as an osmotic agent
in the gut. In the colon, lactulose is broken down by bacteria to lactic, formic,
and acetic acids plus carbon dioxide, which tend to also increase motility.
Phenolphthalein, like anthraquinones and other irritant phenolic
compounds, is a stimulant laxative. Colonic peristalsis is increased by stim-
ulation of sensory nerve endings in the mucosa of the intestine. Phenol-
phthalein also enhances entrance of water and salts into the bowel.

410–411. The answers are 410-i, 411-d. (Hardman, pp 156, 622, 624.)
Misoprostol, a methyl analogue of PGE1, is used in the prevention of ulcers
that are caused by NSAIDs, especially in patients with rheumatoid arthri-
tis. Misoprostol inhibits gastric secretion. Because of its stimulatory effect
on the uterus, it is contraindicated in women of childbearing age.
Prostaglandins, especially PGE2 and PGI2, stimulate inhibitory G protein,
which controls adenylate cyclase, so as to decrease the production of cAMP
and, thus, decrease the action of the H+,K+,ATPase pump through protein
kinase. Aspirin and other NSAIDs inhibit the synthesis of prostaglandins,
allowing stimulatory G protein to be activated by other mechanisms and,
thus, allowing the parietal cell to secrete more acid.